CY 216
Heparin
CAS: 9005-49-6;91449-79-5
Molecular Formula: C26H41NO34S4
CY 216 - Names and Identifiers
CY 216 - Physico-chemical Properties
| Molecular Formula | C26H41NO34S4 |
| Molar Mass | 1134.93 |
| Density | 2.13g/cm3 |
| Melting Point | 250 °C (decomp) |
| Specific Rotation(α) | D20 +55° |
| Solubility | H2O: 50mg/mL, clear, faintly yellow |
| Appearance | crystalline (fine) |
| Color | white |
| Refractive Index | 1.711 |
| Physical and Chemical Properties | Heparin Sodium is a sodium salt of amino dextran sulfate extracted from the intestinal mucosa of pigs or cattle. It is white or off-white powder, odorless, tasteless and has hygroscopicity. Soluble in water, insoluble in ethanol, acetone and other organic solvents. Heparin injection is a sterile aqueous solution of heparin, a colorless or yellowish clear liquid; Heparin chilblain ointment is a white ointment containing heparin sodium. This product was first found in the liver of dogs, so the name heparin. In nature, heparin is widely distributed in the liver, lung, heart, spleen, kidney, thymus, intestinal mucosa, muscle and blood of mammals, and is often combined with proteins to form complexes. This complex has no anticoagulant activity, and the activity increases as the protein is removed. In vivo by the liver to produce heparanase inactivation with urine excretion. Heparin is a sulfate-containing mucopolysaccharide whose molecular structure is represented by a tetrasaccharide repeating unit and whose components are glucosamine, iduronic acid and glucuronic acid. Since the heparin molecule contains sulfate anion which accounts for about 40% of the molecular weight, it has many negative charges. This highly negatively charged physical and chemical property interferes with many links in the blood coagulation process. In addition to the inhibition of the activity of each coagulation factor, the antithrombotic effect of heparin has vascular wall interaction and other factors. In addition, heparin also has hypolipidemic, anti-atherosclerosis, anti-inflammatory, anti-allergic effect, but also to prevent thrombosis, cerebrovascular disease, clear the role of kidney disease formation. |
| In vitro study | Heparin is a potent anticoagulant drug based on its ability to accelerate the rate at which antithrombin inhibits serine proteases in the blood coagulation cascade. Heparin and the structurally related heparan sulfate are complex linear polymers comprised of a mixture of chains of different length, having variable sequences. Heparin interactes most tightly with peptides containing a complementary binding site of high positive charge density. Heparin and heparan sulfate predominantly exhibit linear helical secondary structures with sulfo and carboxyl groups displayed at defined intervals and in defined orientations along the polysaccharide backbone. Heparin resembles DNA as both are highly charged linear polymers that behave as polyelectrolytes. Heparin is believed to function as an anticoagulant primarily through its interaction with AT III by enhancing AT-III-mediated inhibition of blood coagulation factors, including thrombin and factor Xa. Heparin binds to AT III and thrombin in a ternary complex, increasing the bimolecular rate constant for the inhibition of thrombin by a factor of 2000. Heparin is principally located in the granules of tissue mast cells that are closely associated with the immune response. Heparin makes numerous contacts with both FGF-2 and FGFR-1 stabilizing FGF–FGFR binding. Heparin also makes contacts with the FGFR-1 of the adjacent FGF–FGFR complex, thus seeming to promote FGFR dimerization. |
CY 216 - Risk and Safety
| Safety Description | 24/25 - Avoid contact with skin and eyes. |
| WGK Germany | 2 |
| RTECS | MI0850000 |
| FLUKA BRAND F CODES | 3-10 |
| Toxicity | LD50 oral in rat: 1950mg/kg |
